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This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License
Uduma Eke Osonwa, Onyinye Uwaezuoke and Ngozi Ilunoh
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DOI:10.17265/1934-7375/2016.06.006
The aim of this work was to increase the efficacy of erythromycin ethyl succinate by encapsulation in beeswax lipid matrix using Myrj 52 as emulsifier. Different batches of SLM’s (solid-lipid microparticles) were formulated and stable ones were selected. The encapsulation efficiency and loading capacities were calculated. The batch with the highest loading capacity was used for further assays. The particle size was determined by light microscopy. The sensitivity of different clinical bacterial isolates to erythromycin was tested using in vitro cultures and E. coli was selected for efficacy tests. The activity of the formulated drug was tested in the in vitro culture and compared to that of the unformulated drug. White albino mice were infected with E. coli and left for one day to develop significant bacteremia. They were then divided into 4 groups (n = 4) and treated with the formulation and unformulated drug at a dose of 7.14 mg/kg 8 hourly for 56 hours. A third group was given SLM’s that do not contain drug, while another group was left untreated. The selected batch has an encapsulation efficiency of 94.83% with a loading capacity of 3.88%. The particle size was 17 ± 4 µm. At the end of the three day period of treatment, the group treated with unformulated erythromycin had much stooling and weakness in the mice, and some deaths were recorded, while that treated with the formulation had 33.8% bacteremia and the clinical signs had largely subsided. The other two groups recorded deaths the following day after bacteremia induction. The results show marked improvement in efficacy of erythromycin ethyl succinate by formulation in SLMs with beeswax and lecithin as lipid matrix.
Erythromycin, SLM, beeswax-lecithin SLM, E. coli, improved activity.
[1] Kawakami, K., Yoshikawa, T., Hayashi, T., Nishihara, Y., and Masuda, K. 2002. “Microemulsion Formulation for Enhanced Absorption of Poorly Soluble Drugs II.” Journal of controlled Release 81: 75-82.
[2] Amidon, G. L., Lennernäs, H., Shah, V. P., and Crison, J. R. 1995. “A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability.” Pharm. Res. 12 (3): 413-20.
[3] Pramod, R. S., Balasaheb, S. P., Shilpi, R., Sarita, S. R., and Amruta, B. V. 2014. “Approaches towards the Solubility Enhancement of Drug: A Review.” World Journal of Pharmacy and Pharmaceutical Sciences 3 (4): 625-45.
[4] Attama, A. A., Momoh, M. M., and Builders, P. F. 2012. “Lipid Nanoparticulate Drug Delivery System: A Revolution in Dosage form Design and Development. In Recent Advances in Novel Drug Carrier Systems.” Edited by Intech. Retrieved online on March 24, 2016 from http://cdn.intechopen.com/pdfs-wm/40253.pdf.
[5] Benameur, H. 2012. “Lipid Based Dosage Forms—An Emerging Platform for Drug Delivery.” Retrieved on March 24, 2016 from http://www.scribd.com/doc/274195065/Lipid-based-Dosage-Forms-An-EmergingPlatform-for-Drug-Delivery-REVIEW-GOOD.
[6] Umeyor, C. E., Kenechukwu, F. K., Uronnachi, E. M., Osonwa, U. E., and Nwakile, C. D. 2012. “Solid Lipid Microparticles: An Effective Lipid Based Technology for Controlled Drug Delivery.” Am. J. PharmTech Res. 2 (6): 1-18.
[7] Dalpiaz, A., Mezzena. M., Scatturin, A., and Scalia, S. 2008. “Solid Lipid Microparticles for the Stability Enhancement of the Polar Drug N6-Cyclopentyladenosine.” Int. J Pharm. 355: 81-6.
[8] Garud, A. Singh, D., and Garud, N. 2012. “SLN (Solid Lipid Nanoparticles): Method, Characterization and Applications.” International Current Pharmaceutical Journal 1 (11): 384-93.
[9] Fahr, A., and Liu, X. 2007. “Drug Delivery Strategies for Poorly Water-soluble Drugs.” Expert Opinion on Drug Delivery 4 (4): 403-16.
[10] Muller, R. H., Mehnert, W., Lucks, J. S., Schwarz, C., Zur Muhlen, A., Meyhers, H., Freitas, C., and Ruhl, D. 1995. “SLN (Solid Lipid Nanoparticles)—An Alternative Colloidal Carrier System for Controlled Drug Delivery.” Eur. J. Pharm Biopharm. 41: 62-9.
[11] Rupenagunta, A., Somasundaram, I., Ravichandiram, V., Kausalya, J., and Senthilnathan, B. 2011. “Solid Lipid Nanoparticles—A Versatile Carrier System.” J. Pharm Res. 4 (7): 2069-75.
[12] Yang, S., Zhu, J., Lu, Y., Liang, B., and Yang, C. 1999. “Body Distribution of Camptothecin Solid Lipid Nanoparticles after Oral Administration.” Pharm Res 16 (5): 751-7.
[13] Kohno, Y. 2002. “Pharmakokinetics and Metabolism of Macrolides.” In Macrolide Antibiotics: Chemistry, Biology and Practice, edited by Omura, S. London: Academic press, 327-61.
[14] Wilson, J. T, and Van Boxtel, C. J. 1978. “Pharmakokinetics of Erythromycin in Man.’ Antibiot. Chemother 25: 181-203.
[15] Ginsburg, C. M. 1986. “Pharmacology of Erythromycin in Infants and Children.” Pediatr. Infect. Dis. J 5: 124-9.
[16] Diab, R., Jaafar-Maalej, C., Fessi, H., and Maincent, P. 2012. “Engineered Nanoparticulate Drug Delivery Systems: The Next Frontier for Oral Administration?” AAPS Journal 14 (4): 688-702.
[17] Momoh, M. A., Kenechukwu, F. C, Gwarzo, M. S., and Builders, P. F. 2015. “Formulation and Evaluation of Ibubrofen Loaded Liposheres for Effective Oral Delivery.” Dhaka Univ. J. Pharm Sci. 14 (1): 17-27.
[18] Sahu, A. K., Kumar, T., and Jain, V. 2016. “Formulation Optimization of Erythromycin Solid Lipid Nanocarrier Using Response Surface Methodology BioMed Research International, 2014.” Retrieved online on March 24, from file:///C:/Users/Uduma/Downloads/689391.pdf.
[19] Martins, R. M., Siqueira, S., Fonseca, M. V., and Freitas, L. A. P. 2014. “Skin Penetration and Photoprotection of Topical Formulations Containing Benzophenone-3 Solid Lipid Microparticles Prepared by the Solvent-Free Spray-Congealing Technique.” J. Microencapsul 31 (7): 644-53.
[20] Mishra, H., Mishra, D., Mishra, P. K., Nahar, M., Dubey, V., and Jain, D. K. 2010. “Evaluation of Solid Lipid Nanoparticles as Carriers for Delivery of Hepatitis B Surface Antigen for Vaccination Using Subcutaneous Route.” J Pharm Pharmaceut Sci 13 (4): 495-509.
[21] Beyalti, Y., Saglam, N., and Aslim, B. 2002. “Determination of Some Properties of Bacillus Isolated from Soil.” Turk J Biol 26: 41-8.
[22] Al-Waili, N. S. 2005. “Mixture of Honey, Beeswax and Olive Oil Inhibits Growth of Staphylococcus Aureus and Candida Albicans.” Arch Med Res. 36 (1): 10-23.